Compound8cexhibited cytotoxicity at nanomolar range; induced G2/M cell cycle arrest accompanied by apoptosis and down-regulated the levels of Pgp, MRP-1 and GST-π.
In the presence of Ru(phen)Cl or fac-Ir(ppy) under visible-light irradiation, the addition of fluorinated radicals to N-arylacrylamides followed by an intramolecular cyano group insertion cascade cyclization process produced trifluoroalkyl or difluoroalkyl phenanthridine derivatives in moderate to good yields. Three easily available fluoroalkylated reagents CFSOCl, BrCFCOEt and BrCFPO(OEt) were used as the sources of fluorinated radicals.
Regioselective
and stereoselective synthesis of trisubstituted
alkenyl silanes via hydrosilylation is challenging. Herein, we report
the first β-anti-selective addition of silanes
to thioalkynes with B(C6F5)3 as the
catalyst. The reaction shows broad substrate
scope. The products were proven to be useful intermediates to other
trisubstituted alkenyl silanes by Ni-catalyzed stereoretentive cross-coupling
reactions of the C–S bond. A mechanism study suggests that
nucleophilic attack of thioalkyne
to an activated silylium intermediate might be the rate-determining
step.
We present an application of generative adversarial networks (GANs) to reconstruct the sea level of the North Sea using a limited amount of data from tidal gauges (TGs). The application of this technique, which learns how to generate datasets with the same statistics as the training set, is explained in detail to ensure that interested scientists can implement it in similar or different oceanographic cases. Training is performed for all of 2016, and the model is validated on data from three months in 2017 and compared against reconstructions using the Kalman filter approach. Tests with datasets generated by an operational model ("true data") demonstrated that using data from only 19 locations where TGs permanently operate is sufficient to generate an adequate reconstruction of the sea surface height (SSH) in the entire North Sea. The machine learning (ML) approach appeared successful when learning from different sources, which enabled us to feed the network with real observations from TGs and produce high-quality reconstructions of the basin-wide SSH. Individual reconstruction experiments using different combinations of training and target data during the training and validation process demonstrated similarities with data assimilation when errors in the data and model were not handled appropriately. The proposed method demonstrated good skill when analyzing both the full signal and the low frequency variability only. It was demonstrated that GANs are also skillful at learning and replicating processes with multiple time scales. The different skills in different areas of the North Sea are explained by the different signal-tonoise ratios associated with differences in regional dynamics.
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